How Modafinil Restores Control to Narcolepsy Patients

How Modafinil Restores Control to Narcolepsy Patients

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Narcolepsy is a sleep disorder that causes daytime sleepiness. It can be hard for friends and family to understand the condition, especially if they don’t have it themselves. They may think you’re lazy or that you stay up too late at night.

Modafinil 200 Australia is known for its waking effects, and has also been used to treat other disorders such as Alzheimer’s disease, ADHD, idiopathic hypersomnia, myotonic dystrophy, depression, and jet-lag. It has been shown to increase Fos-immunoreactivity in orexin neurons in the perifornical cortex of mice and rats.

Modafinil is a Dopamine Receptor Antagonist

Modafinil, unlike stimulants which increase extracellular dopamine by targeting DA transporters, does not affect basal and K+-evoked release of GABA from cultured cortical neurons (Antonelli et al, 1998).

In human positron emission tomography studies using [11C]raclopride, an antagonist which blocks the transporter binding site, modafinil was shown to decrease both the extracellular and plasma levels of dopamine at therapeutically administered doses of 200 and 400 mg/day in healthy male volunteers.

This finding suggests that the arousal and activity-promoting effects of modafinil in narcolepsy, shift work sleep disorder, and depression may be primarily mediated by its actions on monoamine systems.

Indeed, in a double-blind placebo controlled trial of modafinil added to antidepressants in depressed patients, it was shown to improve performance on a frontal-dependent task (Stroop interference) and in other prefrontal measures.

Modafinil is a Dopamine Receptor Modulator

Modafinil is a non-benzodiazepine wakefulness agent that acts as a dopamine transporter inhibitor. This activity may explain its stimulant effects in humans. It also explains why it has a lower liability to abuse than traditional psychostimulants such as amphetamines and copyright.

Modalert 200 mg increases Fos-immunoreactivity in identified orexin cells in the perifornical area of mice and rats. It also stimulates wakefulness in orexin knockout mice without affecting extracellular dopamine levels. It does, however, inhibit the reuptake of dopamine in these cells.

It is also not a monoamine agonist, and it does not increase locomotor activity in rat and mouse lateral striatum.  It does, however, increase rearing in HT and KO mice. This is similar to the increase in rearing observed with methylphenidate.

Modafinil is a Dopamine D2 Receptor Modulator

Modafinil acts as a dopamine D2 receptor modulator by inhibiting the reuptake of dopamine and increasing its availability. It also stimulates adrenergic neurons in the hypothalamus by increasing the production of wakefulness-promoting peptides. It also increases the activity of orexin neurons in the lateral hypothalamus, which project to the rest of the central nervous system.

Its ability to promote wakefulness, enhance cognition, and brighten mood make it a popular choice among people under stress. In addition, it is well tolerated and does not have a high risk for abuse or addiction. Modafinil is available as a tablet to be taken by mouth, and it is usually taken once per day in the morning.

However, some people have severe allergic reactions to this medication. This reaction is called DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms). If you experience this allergy, stop taking modafinil right away.

Modafinil is a Dopamine D3 Receptor Modulator

The drug modafinil effectively treats EDS in narcolepsy and unlike other stimulants does not produce the rebound hypersomnolence or abuse potential seen with some other compounds. However, modafinil has the disadvantage of causing dry mouth and other minor side effects in some patients.

In a double-blind placebo-controlled study, modafinil significantly improved EDS and decreased the need for sleep during the day in narcolepsy patients. This improvement was associated with increased cognitive performance and may be related to medial prefrontal activation processes identified by low-resolution brain electromagnetic tomography (LORETA).

Modafinil acts as a weak DAT inhibitor through competitive binding to the transporter. This results in a reduction in the transporter-mediated accumulation of DAT and an increase in free DA levels.

Microdialysis studies show that D3 receptors are mainly located in the striatum (including the nucleus accumbens). The results suggest that modulation of D3 receptors contributes to the wake-promoting effects of modafinil.

Modafinil is a Dopamine D4 Receptor Modulator

Modafinil is a central nervous system stimulant that promotes wakefulness in people with sleep disorders such as narcolepsy. It increases alertness and improves performance on tests that measure wakefulness, such as the Maintenance of Wakefulness Test.

It also increases the time people with narcolepsy stay awake during scheduled waking hours. Modafinil also improves the ability to concentrate and makes it easier to think clearly. It is not a cure for narcolepsy, but it may help control symptoms.

Modafinil acts primarily as a dopamine D4 autoreceptor modulator and enhances the actions of catecholamines. It also interacts with the NMDA receptors and modulates locus coeruleus activity. It is eliminated from the body primarily by amide hydrolysis, with a small fraction excreted as the sulfate conjugate in urine. Modafinil does not interact with clonidine or phenytoin and is generally well tolerated.

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